Group of alpha-glucosidase inhibitors and application thereof

A glucosidase and inhibitor technology, applied in the field of medicinal chemistry, can solve the problems of compound separation, inability to further study or apply the market, affecting the application of Ganoderma lucidum extract, etc.

Active Publication Date: 2017-09-08
赵静
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the above-mentioned prior art does not isolate the compound with the described effect, so there is a problem that it cannot be further studied or applied to

Method used

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  • Group of alpha-glucosidase inhibitors and application thereof
  • Group of alpha-glucosidase inhibitors and application thereof
  • Group of alpha-glucosidase inhibitors and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Compound preparation:

[0026] Sessile Ganoderma lucidum was powdered and extracted three times with 95% ethanol for 2 hours each time. The three extracts were combined and concentrated to obtain the extract. The Ganoderma lucidum extract was dissolved in 10% ethanol, loaded on D101 macroporous resin, and eluted with water, 30%, 70%, and 95% ethanol in sequence. The eluate was concentrated to obtain a sample eluting with water (DW), a sample eluting with 30% ethanol (D30), a sample eluting with 70% methanol (D70) and a sample eluting with 95% methanol (D100).

[0027]Different concentrations of Ganoderma lucidum extract were added to the microtiter plate at 20 μL per well, and triplicate wells were set up for each concentration. In addition, a drug control well, a positive reaction well and a positive control well were set up. Then add 20 μL of 0.2 U / mL α-glucosidase to drug reaction wells and positive reaction wells, and add 20 μL phosphate buffer to drug control we...

Embodiment 2

[0037] The 10% ethanol obtained by the operation of Example 1 dissolves the ganoderma lucidum extract, loads the sample on D101 macroporous resin, and successively elutes with 30% and 95% ethanol, and the 95% ethanol eluent recovers the solvent under reduced pressure to obtain the extract. The compound was chromatographed on a 500-800 mesh silica gel column, eluted with a gradient of chloroform-methanol system (100:0-0:100, v / v), and the fractions of the same components were combined to obtain 3 components (Fr1-3) ; Fr1 was subjected to silica gel column chromatography, petroleum ether-acetone (8:1-1:1, v / v) gradient elution to obtain 4 components (Fr1-1~Fr1-4); component Fr1-1 was purified by silica gel Column chromatography column, chloroform-ethyl acetate (30:1, v / v) isocratic elution to obtain compound 1. Component Fr1-2 was subjected to reverse-phase ODS column chromatography, and gradient elution of methanol-water (80:20-100:0, v / v) was used to obtain compound 2. Fr2 wa...

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PUM

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Abstract

The invention relates to application of compounds, which are separated from ganoderma fungi and have alpha-glucosidase inhibiting activity, to medicinal treatment and functional food health care. The alpha-glucosidase inhibiting activity of the compounds or natural or synthetic components containing one or more of the compounds is 1.6-26 times of that of acarbose. The compounds or the components containing the compounds can be prepared into a variety of solid or liquid oral preparations, or through addition of other components and auxiliary materials, compound medicines or health products are prepared and are used for treating and preventing diabetes.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to an alpha-glucosidase inhibitor, in particular to the application of the one or more compounds in the preparation of medicines or health food for treating and preventing diabetes. Background technique [0002] In recent years, due to many factors such as the improvement of living standards, changes in dietary structure, increasingly tense pace of life, and less active and more sedentary lifestyle, the incidence of diabetes worldwide has increased rapidly. Diabetes has become the third largest disease after tumors and cardiovascular diseases. Chronic diseases that seriously threaten human health. In 2014, approximately 422 million people worldwide had diabetes, and the prevalence of diabetes has nearly doubled since 1980, rising from 4.7% to 8.5% in adults. The prevalence of diabetes has risen faster in low- and middle-income countries than in high-income countries o...

Claims

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Application Information

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IPC IPC(8): C07J9/00A61K31/575A61P3/10A23L33/11
Inventor 赵静李绍平陈显强
Owner 赵静
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